Abstract: This invention relates to novel compounds, compositions containing the compounds, that inhibit dipeptidyl peptidase (especially DPP-IV) and neprilysin (NEP, neutral endopeptidase) as well as dipeptidyl peptidase (especially DPP-IV) and angiotensin converting enzyme (ACE) and/or dipeptidyl Peptidase (especially DPP-IV) and vasopeptidases (especially ACE and NEP). These compounds and pharmaceutical compositions thereof are useful for the treatment as well as the prevention of type 2 diabetes mellitus.
Type:
Application
Filed:
August 31, 2004
Publication date:
March 2, 2006
Applicant:
Morphochem AG
Inventors:
Sabine Pierau, Christian Oefner, Glenn Dale
Abstract: The present invention is directed to novel acyloins, their derivatives, methods for their production and their use for the production of novel epothilones and their derivatives. In addition, the invention is directed to the building blocks for epothilone synthesis, methods for their production and the use of synthetic building blocks for the production of epothilones and their derivatives.
Type:
Grant
Filed:
April 15, 2003
Date of Patent:
March 15, 2005
Assignee:
Morphochem AG
Inventors:
Ludger A. Wessjohann, Gunther Scheid, Uwe Bornscheuer, Erik Henke, Wouter Kuit, Romano Orru
Abstract: The present invention relates to compounds of formula (I):
or a pharmaceutically acceptable salt, solvate, hydrate or a pharmaceutically acceptable formulation thereof. Those compounds can be used for inhibiting factor Xa and for the prevention and/or treatment of thromboembolic conditions.
Type:
Grant
Filed:
February 19, 2003
Date of Patent:
September 21, 2004
Assignee:
Morphochem AG
Inventors:
Michael W. Cappi, Thilo Fuchs, Robert Eckl, Silke Schabbert
Abstract: The invention relates to a process for the preparation of heterocycles, characterised in that the following components:
i) a propargyl derivative of the general structural formula I
a wherein Het is an optionally substituted hetero atom and A is a substituted or unsubstituted aromatic entity, a substituted or unsubstituted aromatic heterocycle, a substituted or unsubstituted vinyl arene and/or a derivative thereof, an olefin, an alkyne, an acceptor group or a nitrile;
(ii) a compound of the general structural formula II,
B—X II,
wherein B is an electron-deficient substituted or unsubstituted aromatic entity with or without an acceptor group, an electron-deficient substituted or unsubstituted heteroaromatic entity with or without an acceptor group, an electron-deficient olefin and/or alkyne, a metal complex, and X is a leaving group;
(iii) a nucleophile of the general structural formula III,
Y—Cn—Z III,
wherein Y and/or Z, each
Abstract: The present invention relates to 3-pyrroloimidazole derivatives of the general formula (I)
wherein the imidazole radical is an optionally substituted imidazole ring, X, Y, A and B are, each independently of the others, carbon or nitrogen atoms, the radicals Z denote, each independently of the others, a hydrogen atom, a halogen atom, a pseudohalogen, an optionally substituted alkyl, alkenyl, alkynyl, aralkyl, aralkenyl, aralkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloaralkyl, cycloaralkenyl, cycloaralkynyl, aryl or alkoxy radical or an optionally substituted ring, to which one or two further, optionally substituted rings may be fused, and/or at least two of the radicals Z may be part of an optionally substituted ring, to which one or two further, optionally substituted rings may be fused, and to pharmaceutical compositions comprising at least one of the above-mentioned compounds, optionally in combination with carriers and/or adjuvants and/or excipients customary per se.
Abstract: A process for the preparation of polymers having nucleobases as side groups by means of multicomponent reactions, especially the Ugi reaction, is described. Because of the multicomponent nature of preparation, the properties of the polymers can be varied substantially better than has hitherto been possible and can be adapted to requirements for use as an antisense or antigen therapeutic agent or as a diagnostic agent.